title: Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives.
abstract: A series of new beta-carboline derivatives, bearing a benzylidine substituent at position-1, has been prepared and evaluated in vitro against a panel of human cell lines. The N(2)-benzylated beta-carbolinium bromates represented the most interesting cytotoxic activities. In particular, compounds 19 were found to be the most potent compounds with IC(50) values lower than 5 microM against 10 strains human tumor cell lines. These results confirmed that the N(2)-benzyl substituent on the beta-carboline ring played an important role in the modulation of the cytotoxic activities and suggested that further development of such compounds may be interest.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen (Zhongshan) University, 135 Xin Gang Xi Road, Guangzhou 510275, PR China. caorihui@mail.sysu.edu.cn
authors.forename: Rihui
authors.initials: R
authors.lastname: Cao
authors.forename: Wei
authors.initials: W
authors.lastname: Yi
authors.forename: Qifeng
authors.initials: Q
authors.lastname: Wu
authors.forename: Xiangdong
authors.initials: X
authors.lastname: Guan
authors.forename: Manxiu
authors.initials: M
authors.lastname: Feng
authors.forename: Chunming
authors.initials: C
authors.lastname: Ma
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Chen
authors.forename: Huacan
authors.initials: H
authors.lastname: Song
authors.forename: Wenlie
authors.initials: W
authors.lastname: Peng
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006247:Harmine / Q000138:chemical synthesis* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007477:Ions; D008956:Models, Chemical; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002243:Carbolines; D007477:Ions; D006247:Harmine